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Art. -Nr.: HY-151464

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SHP2/HDAC-IN-1

SHP2/HDAC-IN-1 is a dual allosteric SHP2/HDAC inhibitor with IC₅₀ values of 20.4 nM (SHP2) and 25.3 nM (HDAC1) respectively. SHP2/HDAC-IN-1 triggers efficient antitumor immunity by activating T cells, enhancing the antigen presentation function and promoting cytokine secretion. SHP2/HDAC-IN-1 can be used in the research of cancer immunoresearch.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 2831230-38-5
Formel: C₃₄H₃₅Cl₂N₇O₃
Molecular Weight:660.59

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

SHP2/HDAC-IN-1 Chemical Structure

CAS. Nr.: 2831230-38-5

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

HDAC1

25 nM (IC₅₀)

HDAC2

79 nM (IC₅₀)

HDAC3

233 nM (IC₅₀)

HDAC6

27 nM (IC₅₀)

SHP2

20.4 nM (IC₅₀)

Alle HDAC Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	IC₅₀	5.43 μM Compound: 8t	Antiproliferative activity against mouse 4T1 cells assessed as cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse 4T1 cells assessed as cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36097406]
ASPC1	IC₅₀	2.31 μM Compound: 8t	Antiproliferative activity against human ASPC1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human ASPC1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36097406]
BXPC-3	IC₅₀	1.65 μM Compound: 8t	Antiproliferative activity against human BXPC-3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human BXPC-3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36097406]
KYSE-520 cell line	IC₅₀	1.95 μM Compound: 8t	Antiproliferative activity against human KYSE520 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human KYSE520 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36097406]
MV4-11	IC₅₀	0.07 μM Compound: 8t	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36097406]
SW1990	IC₅₀	3.92 μM Compound: 8t	Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36097406]

In Vitro

SHP2/HDAC-IN-1 (compound 8t, 0-10 μM approximately, 72 h) inhibits the proliferation of BxPC-3, SW1990, AsPC-1and MV4-11 cells^[1].
SHP2/HDAC-IN-1 (0.25-1 μM, 24 h) increases the acetylation of α-tubulin and histone H3 in MV4-11 cells^[1].
SHP2/HDAC-IN-1 (0.25 μM, 24 h) inhibits cell cycle progression in the G1 phase of MV4-11 cells^[1].
SHP2/HDAC-IN-1 (0.25 and 0.5 μM, 24 h) decreases the mitochondrial membrane potential and activats caspase-3^[1].
SHP2/HDAC-IN-1 (2 h) shows good stability in in mouse liver microsome^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

Pancreatic carcinoma (BxPC-3, SW1990, and AsPC-1), acute monocytic leukemia (MV4-11)
Concentration:

0-10 μM approximately
Incubation Time:

72 h
Result:

Inhibited cell proliferation with IC₅₀s range of 0.07 μM-3.92 μM.

Western Blot Analysis^[1]

Cell Line:

MV4-11 cells
Concentration:

0.25, 0.5, 1 μM
Incubation Time:

24 h
Result:

Increased the acetylation of α-tubulin and histone H3.
Inhibited the phosphorylation level of ERK.

In Vivo

SHP2/HDAC-IN-1 (compound 8t, 40 mg/kg, p.o.) inhibits tumor growth in MV4-11 and 4T1 tumor-bearing xenograft mice^[1].
SHP2/HDAC-IN-1 (20 mg/kg p.o., 1 mg/kg i.v.) exhibits good maximum plasma concentrations in rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

MV4-11 tumor-bearing xenograft mice^[1]
Dosage:

40 mg/kg
Administration:

Oral adminstration (p.o.), every day for 20 consecutive days.
Result:

Delayed tumor progression with a tumor growth inhibition rate (TGI %) value of 64.0%, with no obvious signs of toxicity.

Animal Model:

4T1 murine breast cancer model^[1]
Dosage:

40 mg/kg
Administration:

Oral adminstration (p.o.), every day for 12 consecutive days.
Result:

Significantly decreased tumor burden with a TGI value of 72%.
Increased the proportions of CD4+ T cells and CD8+ T cells in the spleen.
Enhanced the proportion of mDCs in lymph nodes.

Animal Model:

Male Sprague-Dawley (SD) rats (Pharmacokinetic assay)^[1]
Dosage:

20 mg/kg p.o., 1 mg/kg i.v.
Administration:

Oral adminstration (p.o.) or intravenous injection (i.v.)
Result:

Pharmacokinetic profile of SHP2/HDAC-IN-1 (compound 8t).

dose (mg/kg) T_1/2 (h) C_max (ng/mL) Cl (mL/h/kg) F (%)

20 (p.o.) 5.32 1835 21.42

1 (i.v.) 6.15 3517 326

Related Protocols :

Chemical Information

CAS. Nr. 2831230-38-5
Molecular Weight 660.59
Formel C₃₄H₃₅Cl₂N₇O₃
SMILES

O=C(NCC1=CC=C(/C=C/C(NO)=O)C=C1)C2=CC=C(CNC3(C)CCN(C4=NC(N)=C(C5=C(Cl)C(Cl)=CC=C5)N=C4)CC3)C=C2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Meng Liu, et al. Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity. J Med Chem. 2022 Sep 22;65(18):12200-12218. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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